Pardoprunox

Alias: Pardoprunox; SLV-308; SLV 308; SLV308; DU-126891; DU126891; DU 126891; SME-308; SME308; SME308

Cat No.:V3783 Purity: ≥98%

COA Product Data Instructions for use SDS

Pardoprunox (formerly known as SLV-308, DU-126891 or SME-308) is novel & potent dopamine D2/5-HT1A receptor agonist that has the potential for the treatment of Parkinson's disease.

Pardoprunox Chemical Structure CAS No.: 269718-84-5
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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1-708-310-1919 sales@invivochem.com

Other Forms of Pardoprunox:

Pardoprunox HCI

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Pardoprunox (formerly known as SLV-308, DU-126891 or SME-308) is novel & potent dopamine D2/5-HT1A receptor agonist that has the potential for the treatment of Parkinson's disease. Pardoprunox acts by binding to dopamine D(2), D(3), and D(4) receptors and 5-HT(1) (A) receptors and is a partial agonist at dopamine D(2) and D(3) receptors and a full agonist at serotonin 5-HT(1) (A) receptors. SLV308 functioned as a strong but partial D(2) receptor agonist at cloned human dopamine D(2,L) receptors (pEC(50) = 8.0 and pA(2) = 8.4) with a 50% efficacy on forskolin stimulated cAMP accumulation. SLV308 functioned as a partial agonist at human recombinant dopamine D(3) receptors, inducing [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and inhibiting the dopamine-induced [(35)S]GTPgammaS binding (pA(2) = 9.0). On forskolin-induced cAMP accumulation at cloned human 5-HT(1) (A) receptors, SLV308 functioned as a full 5-HT(1) (A) receptor agonist, albeit with low potency (pEC(50) = 6.3).

Biological Activity I Assay Protocols (From Reference)

Targets

5-HT_1A Receptor ( pEC50 = 6.3 ); D₂ Receptor ( pEC50 = 8 ); D₃ Receptor ( pEC50 = 9.2 )

ln Vitro

In vitro activity: Pardoprunox (SLV-308) has a 50% efficacy on forskolin-stimulated cAMP accumulation and functions as a strong but partial D2 receptor agonist (pEC50= 8.0 and pA2= 8.4). At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC50=9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA2=9.0). On forskolin-induced cAMP accumulation at cloned human 5-HT1A receptors, pardoprunox functions as a full 5-HT1A receptor agonist, albeit with low potency (pEC50=6.3)[1].

ln Vivo

Pardoprunox induces contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In MPTP-treated common marmosets, Pardoprunox dose-dependently increases locomotor activity (MED=0.03mg/kg; po) and decreases motor disability (MED=0.03mg/kg; po). In contrast Pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphine-induced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induces 5-HT1A receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po). Collectively, these findings demonstrate that Pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. functional D2 receptor partial agonist activity and is effective in experimental models predictive of efficacy in PD

Animal Protocol

0.03mg/kg; po

Rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc)

References

[1]. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608.

[2]. Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease. Mov Disord. 2010 Apr 30;25(6):738-46.

[3]. In vivo effects of pardoprunox (SLV308), a partial D?/D? receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C12H15N3O2

Molecular Weight

233.27

Exact Mass

233.12

Elemental Analysis

C, 61.79; H, 6.48; N, 18.01; O, 13.72

CAS #

269718-84-5

Related CAS #

Pardoprunox hydrochloride; 269718-83-4

Appearance

Solid powder

SMILES

CN1CCN(CC1)C2=CC=CC3=C2OC(=O)N3

InChi Key

YVPUUUDAZYFFQT-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H15N3O2/c1-14-5-7-15(8-6-14)10-4-2-3-9-11(10)17-12(16)13-9/h2-4H,5-8H2,1H3,(H,13,16)

Chemical Name

7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one

Synonyms

Pardoprunox; SLV-308; SLV 308; SLV308; DU-126891; DU126891; DU 126891; SME-308; SME308; SME308

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~10 mM

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

O=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.2869 mL	21.4344 mL	42.8688 mL
	5 mM	0.8574 mL	4.2869 mL	8.5738 mL
	10 mM	0.4287 mL	2.1434 mL	4.2869 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00335374	Completed	Drug: Pardoprunox	Early Stage Parkinson's Disease	Solvay Pharmaceuticals	August 2007	Phase 3
NCT00332917	Completed	Drug: Pardoprunox	Early Stage Parkinson's Disease	Solvay Pharmaceuticals	February 2007	Phase 3
NCT00407095	Completed	Drug: Pardoprunox	Advanced Stage Parkinson's Disease	Solvay Pharmaceuticals	August 2007	Phase 3
NCT00406588	Completed	Drug: Placebo Comparator Drug: Levodopa (Pardoprunox)	Advanced Stage Parkinson's Disease	Solvay Pharmaceuticals	March 2007	Phase 3
NCT00269516	Completed	Drug: pardoprunox Drug: Placebo	Early Stage Parkinson's Disease	Solvay Pharmaceuticals	June 2006	Phase 3